Page last updated: 2024-08-07 23:52:07
Rhodopsin kinase GRK1
A rhodopsin kinase GRK1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15835]
Synonyms
RK;
EC 2.7.11.14;
G protein-coupled receptor kinase 1
Research
Bioassay Publications (7)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (28.57) | 29.6817 |
| 2010's | 5 (71.43) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (72)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nsc 65346 | Homo sapiens (human) | Ki | 0.1800 | 1 | 1 |
| paroxetine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0680 | 2 | 2 |
| ophiocordin | Homo sapiens (human) | IC50 | 0.3400 | 1 | 1 |
Drugs with Activation Measurements
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| rhodopsin kinase activity | molecular function | Catalysis of the reaction: ATP + rhodopsin = ADP + phosphorhodopsin. [PMID:14654303] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| photoreceptor disc membrane | cellular component | Stack of disc membranes located inside a photoreceptor outer segment, and containing densely packed molecules of photoreceptor proteins that traverse the lipid bilayer. Disc membranes arise as evaginations of the ciliary membrane during the development of the outer segment and may or may not remain contiguous with the ciliary membrane. [GOC:bj, GOC:krc, GOC:pde, PMID:11826267, PMID:19501669, PMID:2537204, PMID:26574505, PMID:6771304, PMID:7507907] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| visual perception | biological process | The series of events required for an organism to receive a visual stimulus, convert it to a molecular signal, and recognize and characterize the signal. Visual stimuli are detected in the form of photons and are processed to form an image. [GOC:ai] |
| regulation of G protein-coupled receptor signaling pathway | biological process | Any process that modulates the frequency, rate or extent of G protein-coupled receptor signaling pathway. [GOC:go_curators] |
| rhodopsin mediated signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by the excitation of rhodopsin by a photon, and ending with the regulation of a downstream cellular process. [GOC:bf, GOC:dph, GOC:hb, GOC:signaling, GOC:tb] |
| regulation of opsin-mediated signaling pathway | biological process | Any process that modulates the frequency, rate or extent of opsin-mediated signaling. [GOC:mah] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| regulation of signal transduction | biological process | Any process that modulates the frequency, rate or extent of signal transduction. [GOC:sm] |